在大鼠体内具有增强溶解度、溶解度和生物利用度的亲水性聚合物组成的头孢地尼固体分散体

Hyun-Jong Cho, Jun-Pil Jee, Ji-Ye Kang, D. Shin, Han‐Gon Choi, H. Maeng, K. Cho
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引用次数: 18

摘要

本工作的目的是开发头孢地尼固体分散体(CSDs)制备的亲水聚合物具有提高溶解/溶解度和体内口服生物利用度。以羟丙基甲基纤维素(HPMC;CSD1),羧甲基纤维素- na (CMC-Na;CSD2)、聚乙烯吡咯烷酮K30 (PVP K30;CSD3)以1:1的重量比(药物:聚合物)采用喷雾干燥方法。通过水溶性、差示扫描量热法(DSC)、粉末x射线衍射(p-XRD)、扫描电镜(SEM)、水黏度和在各种介质中的溶解试验对制备的CSDs进行了表征。并与头孢地尼粉末混悬液比较,评价了CSDs在大鼠体内的口服生物利用度。经DSC和p-XRD测定证实,CSDs中的头孢地尼为无定形。与头孢地尼结晶粉末相比,开发的CSDs通常使头孢地尼的溶解度提高约9.0倍,并且在水和pH为1.2时的溶解谱显着改善。重要的是,与头孢地尼混悬液相比,CSD1、CSD2和CSD3在大鼠体内的口服吸收(用AUCinf表示)分别显著增加4.30倍、6.77倍和3.01倍。CMC-Na制备的CSD2是提高头孢地尼体内溶出度和生物利用度的有效载体。
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Cefdinir Solid Dispersion Composed of Hydrophilic Polymers with Enhanced Solubility, Dissolution, and Bioavailability in Rats
The aim of this work was to develop cefdinir solid dispersions (CSDs) prepared using hydrophilic polymers with enhanced dissolution/solubility and in vivo oral bioavailability. CSDs were prepared with hydrophilic polymers such as hydroxypropyl-methylcellulose (HPMC; CSD1), carboxymethylcellulose-Na (CMC-Na; CSD2), polyvinyl pyrrolidone K30 (PVP K30; CSD3) at the weight ratio of 1:1 (drug:polymer) using a spray-drying method. The prepared CSDs were characterized by aqueous solubility, differential scanning calorimetry (DSC), powder X-ray diffraction (p-XRD), scanning electron microscopy (SEM), aqueous viscosity, and dissolution test in various media. The oral bioavailability of CSDs was also evaluated in rats and compared with cefdinir powder suspension. The cefdinir in CSDs was amorphous form, as confirmed in the DSC and p-XRD measurements. The developed CSDs commonly resulted in about 9.0-fold higher solubility of cefdinir and a significantly improved dissolution profile in water and at pH 1.2, compared with cefdinir crystalline powder. Importantly, the in vivo oral absorption (represented as AUCinf) was markedly increased by 4.30-, 6.77- and 3.01-fold for CSD1, CSD2, and CSD3, respectively, compared with cefdinir suspension in rats. The CSD2 prepared with CMC-Na would provide a promising vehicle to enhance dissolution and bioavailability of cefdinir in vivo.
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